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Updated: Sep 26, 2026

Nanomechanics of Drug-target Interactions and Antibacterial Resistance Detection
Published on: October 25, 2013
Glycopeptide carboxamides active against vancomycin-resistant enterococci
Mark J Zweifel1, Nancy J Snyder, Robin D G Cooper
1Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA. ZWEIFEL_MARK_J@LILLY.COM
Abstract:
Glycopeptide antibiotics were synthesized via the PyBOP mediated condensation of aliphatic, heterocyclic and aromatic amines with the C-terminus of vancomycin, LY264826 (A82846B) and semi-synthetic derivatives of these natural products. Amides of LY264826 and vancomycin demonstrated excellent activity against staphylococci and streptococci as compared to the parent natural product. However, the amides of N-alkylated LY264826 and N-alkylated vancomycin were active against vancomycin-resistant enterococci as well as other gram-positive pathogens such as Staphylococcus aureus, S. haemolyticus, S. epidermidis and Streptococcus pneumoniae.
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